PL120131 acetate is a PD-1 antagonist, can specifically blocking the interaction between PD-1 and PD-L1, thereby effectively inhibiting the PD-1-mediated apoptosis signaling pathway. PL120131 acetate rescues lymphocytes from apoptosis, maintains the survival and activity of T cells, and induces cytotoxic T lymphocytes to exert killing effects and recognize macrophages and dendritic cells. PL120131 acetate can be used in research related to breast cancer and various malignant tumors [1] [2] [3] [4].
In Vitro, PL120131 acetate (32.0-33.4 μM) rescues Jurkat cells from PD-L1-induced apoptosis, reducing apoptotic signals by 25% with an IC50 of 32.0 μM (Annexin V) and 33.4 μM (Caspase 3/7)[2]. PL120131 acetate (11.6 μM; 24 h) rescues primary mouse T-cells from apoptosis in 4T1 co-cultures, increases 4T1 cell death, and induces a significant, dose-dependent increase in Granzyme B production in CD3+/CD8+ T-cells[2]. PL120131 acetate (0.2-12.5 μg/mL; 24 h) induces dose-dependent increases in IFNγ and dose-dependent decreases in IL-12p70 and IL-10 in co-cultures of primary mouse lymphocytes and 4T1 cells, indicating activated T-cell function[2]. PL120131 acetate (30 μM; 30 min (Jurkat pre-treatment); 24 h (co-culture in microfluidics chip)) enables Jurkat cells to infiltrate a 3D MDA-MB-231 tumor environment, induce greater tumor cell death, and maintain higher Jurkat cell viability than anti-PD-1 antibody treatment[2].
References:
[1]. Tseng T S, et al. Structure-guided discovery of PD-1/PD-L1 interaction inhibitors: peptide design, screening, and optimization via computation-aided phage display engineering[J]. Journal of Chemical Information and Modeling, 2024, 64(5): 1615-1627.
[2]. Boohaker R J, et al. Rational design and development of a peptide inhibitor for the PD-1/PD-L1 interaction[J]. Cancer letters, 2018, 434: 11-21.
[3]. Gu W, et al. Undo the brake of tumour immune tolerance with antibodies, peptide mimetics and small molecule compounds targeting PD‐1/PD‐L1 checkpoint at different locations for acceleration of cytotoxic immunity to cancer cells[J]. Clinical and Experimental Pharmacology and Physiology, 2019, 46(2): 105-115.
[4]. Sun M, et al. Fibroblast Activation Protein-α Responsive Peptide Assembling Prodrug Nanoparticles for Remodeling the Immunosuppressive Microenvironment and Boosting Cancer Immunotherapy. Small. 2022;18(9):e2106296.
In Vitro, PL120131 acetate (32.0-33.4 μM) rescues Jurkat cells from PD-L1-induced apoptosis, reducing apoptotic signals by 25% with an IC50 of 32.0 μM (Annexin V) and 33.4 μM (Caspase 3/7)[2]. PL120131 acetate (11.6 μM; 24 h) rescues primary mouse T-cells from apoptosis in 4T1 co-cultures, increases 4T1 cell death, and induces a significant, dose-dependent increase in Granzyme B production in CD3+/CD8+ T-cells[2]. PL120131 acetate (0.2-12.5 μg/mL; 24 h) induces dose-dependent increases in IFNγ and dose-dependent decreases in IL-12p70 and IL-10 in co-cultures of primary mouse lymphocytes and 4T1 cells, indicating activated T-cell function[2]. PL120131 acetate (30 μM; 30 min (Jurkat pre-treatment); 24 h (co-culture in microfluidics chip)) enables Jurkat cells to infiltrate a 3D MDA-MB-231 tumor environment, induce greater tumor cell death, and maintain higher Jurkat cell viability than anti-PD-1 antibody treatment[2].
References:
[1]. Tseng T S, et al. Structure-guided discovery of PD-1/PD-L1 interaction inhibitors: peptide design, screening, and optimization via computation-aided phage display engineering[J]. Journal of Chemical Information and Modeling, 2024, 64(5): 1615-1627.
[2]. Boohaker R J, et al. Rational design and development of a peptide inhibitor for the PD-1/PD-L1 interaction[J]. Cancer letters, 2018, 434: 11-21.
[3]. Gu W, et al. Undo the brake of tumour immune tolerance with antibodies, peptide mimetics and small molecule compounds targeting PD‐1/PD‐L1 checkpoint at different locations for acceleration of cytotoxic immunity to cancer cells[J]. Clinical and Experimental Pharmacology and Physiology, 2019, 46(2): 105-115.
[4]. Sun M, et al. Fibroblast Activation Protein-α Responsive Peptide Assembling Prodrug Nanoparticles for Remodeling the Immunosuppressive Microenvironment and Boosting Cancer Immunotherapy. Small. 2022;18(9):e2106296.